Rivastigmine



Better Known as: Exelon

 * Marketed By: Novartis


 * Major Indication: Alzheimer's Disease


 * Drug Class: Acetylcholinesterase Inhibitor
 * Date of FDA Approval (Patent Expiration): 2007 (


 * 2006 Sales: $220 Million
 * Importance: One of the the first treatments for the symptoms of Alzheimer's Disease, although no definitive proof exists as to whether it alters the progression of the disease.
 * See: Pharmaceutical Drugs for more information about other drugs and disorders

Mechanism of Action
Rivastigmine is an Acetylcholinesterase (AChE) inhibitor. It binds to the active site of AChE, utilizing many of the same residues which bind and break down acetylcholine. By inhibiting AChE, the important neurotransmitter, acetylcholine, is degraded at a slower rate, helping reverse the marked decrease in neuronal function evident in Alzheimer's Disease patients. Rivastigmine is rapidly metabolized into its principal components (carbamyl and NAP moieties) which are powerful Acetylcholine inhibitors. These components primarily primarily interact with residues GLy 117, Gly 118, Gly 119 Ala 201, Trp 233, Phe 290, Trp 84, Phe 330, His 440, & Phe 288 in tightly binding to the AChE binding site via pi stacking and hydrogen bond interactions. Rivastigmine outcompetes acetylcholine for the active site of AChE, inhibiting the esterase.